1. GPCR/G Protein
  2. Adenosine Receptor
  3. TRR469

TRR469 is a positive allosteric modulator of the A1 adenosine receptor (A1AR). TRR469 significantly increases the affinity of 2-chloro N(6)-cyclopentyladenosine (CCPA) for A₁AR, increasing the number of receptors recognized by the agonist radioligand [³H]-CCPA. TRR469 shows significant effects in both anxiety and pain models. TRR469 can be used to study anxiety disorders and pain management.

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TRR469

TRR469 Chemical Structure

CAS No. : 1394867-58-3

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Description

TRR469 is a positive allosteric modulator of the A1 adenosine receptor (A1AR). TRR469 significantly increases the affinity of 2-chloro N(6)-cyclopentyladenosine (CCPA) for A₁AR, increasing the number of receptors recognized by the agonist radioligand [³H]-CCPA. TRR469 shows significant effects in both anxiety and pain models. TRR469 can be used to study anxiety disorders and pain management[1][2].

In Vitro

TRR469 (10 μM) inhibits the release of excitatory neurotransmitters by enhancing the activation of A₁AR in the spinal cord of mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TRR469 (0.01-3 mg/kg, i.p., single dose) has a significant analgesic effect on acute inflammatory pain, chemical pain and mechanical abnormal pain in mice[1].
TRR469 (0.3-3 mg/kg, i.p., single dose) demonstrates dose-dependent anti-anxiety effects in all four anxiety models[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Formalin test, writhing test, and diabetic neuropathic pain model established in CD-1 mice[1]
Dosage: 0.01, 0.03, 1 and 3 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Showed dose-dependent analgesic effect with ED50s of 0.257 and 0.171 mg/kg in formalin test and writhing test.
Dose-dependent reversaled mechanical abnormal pain.
Animal Model: Elevated cross maze test, the light-dark box test, the opening test and the buried pearl test established in CD-1 mice[2]
Dosage: 0.3, 1 and 3 mg/kg
Administration: Intraperitoneal injection (i.p.), single dose
Result: Demonstrated dose-dependent anti-anxiety effects in all four anxiety models.
Did not enhance the sedative effect of ethanol, nor does it impair the motor coordination function.
Molecular Weight

506.03

Formula

C28H25ClFN3OS

CAS No.
SMILES

O=C(C1=C(N)SC(C2=CC=C(F)C=C2)=C1CN3CCN(C4=CC=CC=C4)CC3)C5=CC=C(Cl)C=C5

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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TRR469 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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TRR469
Cat. No.:
HY-112567
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